Synthesis and biological evaluation of benzimidazole derivatives as potent AMP-activated protein kinase activators

Design, synthesis and structure–activity relationships of benzimidazole derivatives as activators of the AMP-activated protein kinase (AMPK) are presented in this paper. AMPK is the central component of a protein kinase cascade that plays a key role in the regulation of energy balance. Once activated, AMPK initiates a series of responses that are aimed at restoring the energy balance of the cell and recent studies have indicated that AMPK plays an important role in regulation of the whole-body energy metabolism. The following study based on the lead compound S27847 involved modification of three regions of this compound. Preliminary structure–activity relationships are being described.

Design, synthesis and structure–activity relationships of benzimidazole derivatives as activators of the AMP-activated protein kinase are presented in this paper.Figure optionsDownload as PowerPoint slide